Department of Chemistry, University of Delhi, Delhi 110007, India.
Department of Chemistry, University of Delhi, Delhi 110007, India.
Int J Biol Macromol. 2019 Jan;121:6-12. doi: 10.1016/j.ijbiomac.2018.10.005. Epub 2018 Oct 2.
Casein, a milk protein that self-assembles to form micelles in aqueous solution, can bind to a wide range of drugs (hydrophilic and hydrophobic). Herein, a low cost and facile method was reported to prepare casein nanoparticles loaded with an anticancer drug, doxorubicin (DOX). The particles were fabricated by adding an excess of Ca ions which brings the soluble casein present in the solution into the micellar framework to form dense nanoparticles. The binding between the drug and the macromolecule was confirmed using fluorescence studies. Circular Dichroism (CD) shows that upon addition of excess Ca the protein chains rearrange. The nanoparticles were characterized by transmission electron microscopy (TEM), field emission scanning electron microscopy (FESEM), and dynamic light scattering (DLS). The release at pH 1 was higher than the physiological pH making this formulation potent for delivering the drug to the stomach via the oral route. The DOX attached with casein showed improved efficacy, i.e., better cytotoxicity against human pancreatic carcinoma cell line, PANC 1 cells as compared to the free drug of the same concentration, owing to higher cell uptake of the macromolecule.
酪蛋白是一种在水溶液中自组装形成胶束的牛奶蛋白，可以结合广泛的药物（亲水性和疏水性）。本文报道了一种低成本、简便的方法，用于制备载有抗癌药物阿霉素（DOX）的酪蛋白纳米粒。通过添加过量的 Ca 离子来制备纳米粒，将溶液中存在的可溶酪蛋白带入胶束结构中，形成致密的纳米粒。使用荧光研究证实了药物与大分子之间的结合。圆二色性（CD）表明，加入过量的 Ca 后，蛋白质链重新排列。通过透射电子显微镜（TEM）、场发射扫描电子显微镜（FESEM）和动态光散射（DLS）对纳米粒进行了表征。在 pH 1 时的释放量高于生理 pH 值，使得这种制剂通过口服途径将药物递送到胃部具有很强的效力。与相同浓度的游离药物相比，与酪蛋白结合的 DOX 显示出更好的疗效，即对人胰腺癌细胞系 PANC 1 细胞的细胞毒性更好，这是由于细胞对大分子的摄取增加。
